Field of the invention
[0001] This invention relates to a topical antiperspirant composition containing an anticholinergic
agent as the active antiperspirant compound that is substantially free of aluminum
salts.
Background of the Invention
[0002] Antiperspirant and deodorant compositions are widely employed throughout many parts
of the world in order to control localized perspiration and odor. Wet patches such
as those under the arms are considered to be unsightly. Additionally, body odor can
interfere with normal relationships and cause social exclusion. These issues take
on a greater significance particularly in regions that tend to have high humidity
and warmer climates. Besides the underarm area, other body areas including the feet
may benefit from the use of antiperspirants and deodorants.
[0003] Antiperspirants act by stopping or reducing the activity of the sweat glands. Today,
antiperspirants are typically sold in a rollerball applicator or solid stick form
and include an aluminum-based compound, wax, liquid emollients and natural scent enhancers.
Antiperspirants currently marketed commonly employ an astringent metal salt, such
as aluminum or aluminum/zirconium salt. The key to the sweat-blocking activity rests
purely in the active aluminum-based compound that, in a typical commercial antiperspirant,
makes up from about 10 to 25 percent of the ingredients. Aluminum ions, from aluminum
salts such as aluminum chlorohydrate and aluminum chloride, are drawn into the cells
that line the human body's eccrine gland ducts. The eccrine glands are responsible
for producing the majority of the body's sweat and are located in the armpits. The
aluminum ions are taken into the cells that line the eccrine-gland ducts at the opening
of the epidermis, the top layer of the skin. When the aluminum ions are drawn into
the cells, water passes in with them. As more water flows in, the cells begin to swell,
squeezing the ducts closed. Consequently, sweat is directly blocked from being excreted
through the skin. Once the eccrine ducts have been closed, the other odor-reducing/masking
ingredients provide a thin coating to the skin's top layer. The gland ducts remain
closed until the water content outside and inside the gland cells reaches equilibrium
at which time the cell content begins to pass back out through osmosis.
[0004] Deodorants on the other hand block the odor of sweat. Deodorant agents do this by
limiting bacterial proliferation, blocking sweat diffusion, absorbing malodors and
enzymatic inhibition. Commercial products may be marketed as a deodorant, an antiperspirant
or both.
[0005] U.S. Patent Publication No. 2011/0020415 relates to a composition for the treatment of hyperhidrosis. It contains an antiperspirant,
at least one muscle relaxing agent, at least one peptide, and at least one botanical
agent. The antiperspirant is preferably aluminum tertacholrohydrex glycine, and the
peptide may be for example dipeptide diaminobutyroyl benzylamide diacetate, argireline,
SYN-AKE, SNAP 8, or the like.
[0006] Recently, the use of aluminum in deodorants and antiperspirants has become controversial
due to concern that aluminum can be absorbed by the body and enter into the bloodstream.
Additionally, antiperspirant aerosols containing aluminum allow for inhalation during
manufacture and application.
[0007] The present invention provides a novel topical antiperspirant product that does not
require aluminum salts. These antiperspirant compositions are substantially free,
preferably 100% free, of aluminum salts.
Summary of the Invention
[0008] The present invention provides a topical antiperspirant composition comprising a
cosmetically acceptable topical carrier and an anticholinergic agent selected from
the group consisting of acetyl octapeptide-3 and dipeptide diaminobutyroyl benzylamide
diacetate in an amount effective to inhibit or prevent perspiration, wherein said
composition is substantially free of aluminum salts.
[0009] As used herein, the term "comprising" encompasses "including" as well as "consisting"
and "consisting essentially of" e.g. a composition "comprising" X may consist exclusively
of X or may include an additional component, e.g. X + Y.
Detailed Description of the Invention
[0010] The cosmetic antiperspirant composition of the invention is adapted to be applied
topically to a user's skin, typically in the underarm area.
[0011] The composition is substantially free of aluminum salts. In particular, the composition
is substantially free of aluminum chlorohydrate and/or its derivatives. The formulations
may occasionally contain aluminum residue. This is related to traces or extremely
low amounts of aluminum element as a residue in raw materials used as ingredients
of the composition. This is not an aluminum salt.
[0012] As used herein, "substantially free of" an ingredient means containing less than
about 50 ppm in final formulation.
[0013] In one embodiment, the composition of the invention is totally free of aluminum salts.
Anti-cholinergic Agents
[0014] The anti-cholinergic agent in the composition is acetyl octapeptide-3 (for example
SNAP 8 commercially available from Lipotec SA) or dipeptide diaminobutyroyl benzylamide
diacetate (for example SYN-AKE commercially available from Pentapharm Ltd.).
[0015] While not wishing to be being bound by theory, it is believed that dipeptide diaminobutyroyl
benzylamide diacetate acts by blocking the acetylcholine receptor of sweat glands,
while acetyl octapeptide-3 acts by preventing the release of acetylcholine from sympathetic
neurons.
[0016] The anticholinergic agent is present in the composition in an amount effective to
inhibit or substantially reduce perspiration, for example in the underarm area of
a human user following topical application to the same. The composition will generally
contain about 0.01 to about 30.0 w/w% of the anticholinergic agent.
[0017] In one embodiment the composition contains about 0.1 to about 20.0 w/w%, or about
0.5 to about 15.0 w/w%, of acetyl octapeptide-3.
[0018] In another embodiment the composition contains about 0.05 to about 6.0 w/w%, or about
0.1 to about 4.0 w/w%, of dipeptide diaminobutyroyl benzylamide diacetate.
[0019] The composition may optionally also comprise one or more other anticholinergic agents,
including for example biopeptides such as pentapeptide, hexapeptide, or octapeptide,
botulinum toxin (botox), acetyl hexapeptide-8, trihexyphenidyl (artane), benztropine
mesylate (cogentin), biperiden, procyclidine, 2,5 antihistamines (orphenadrine), atropine,
flavoxate (urispas), oxybutynin (ditropan, oxytrol), scopolamine, hyoscyamine (levsinex),
tolterodine (detrol), belladonna alkaloids , fesoterodine (toviaz), solifenacin (vesicare),
darifenacin (enablex), propantheline (pro-banthine).
Water Absorbing Agent
[0020] The composition may optionally comprise a water absorbing agent. Such water absorbing
agents are known for cosmetic applications and are usually porous ingredients, composed
of micro channels resulting in a high absorption capacity and the ability to absorb
a different variety of materials. Such compounds may have affinity to hydrophilic
or lipophilic molecules. In some cases, it is preferred to combine multiple water
absorbing agents in order to maximize the absorption capabilities.
[0021] Suitable water absorbers include silicas, cotton powder, bamboo silk and zeolites.
[0022] In one embodiment, the composition comprises Bambusa Arundinacea Stem Powder (for
example BAMBOO SILK PW available from Polytechno Indústrias Químicas Ltda/lon Química),
silicas (for example MSS 500/3H available from Kobo and/or SPHERON L-1500 available
from Presperse).
[0023] The cosmetic antiperspirant compositions of the present invention will generally
contain from about 0.01 to about 20.0 w/w% of a water absorbing agent in the final
composition. In a preferred embodiment, the composition will contain about 0.1 to
about 10.0 w/w% and in a more preferred embodiment, the cosmetic antiperspirant composition
will contain about 0.5 to about 6.0 w/w% of a water absorbing agent.
[0024] The composition may comprise other ingredients known in the antiperspirant, deodorant,
or cosmetic art. In most embodiments, the antiperspirant will include other functional
ingredients, which provide benefits to the user's body. Such materials are in general
well-known to those persons of ordinary skill in the relevant personal care composition
art, and may include moisturizing agents, anti-bacterial agents, deodorants and perfumes.
[0025] Other ingredients may include film formers. For example, water-insoluble films of
polymers create occlusion on the axillary skin, thereby reducing the underarm wetness.
Such films are a barrier to the passage of sweat. Polymers used should be occlusive,
insoluble in water, and high in degree of adhesion, such as Acrylates/Octylacrylamide
Copolymer.
[0026] The composition may also include ingredients known to have antibacterial and deodorant
properties. These substances may include, for example, 1,6-di-(4-chlorophenylbiguanido)
hexane (Chlorhexidin), 3,4,4'-trichlorocarbanilide, quaternary ammonium compounds,
oil of cloves, mint oil, thyme oil, triethyl citrate, farnesol (3,7,11-trimethyl-2,6,10-dodecatrien-1-ol),
ethylhexyl glycerol ether, or polyglyceryl-3 caprylate. In particular, polyglyceryl
3 caprylate (TEGO® Cosmo P 813, available from Degussa/Evonik), a vegetable sourced
ester, with lipophilic character, may be used to reduce odor-causing bacteria on the
skin at very low concentrations.
[0027] The composition may also comprise linear chain alcohols, amines, ether-alcohols,
cetyl alcohol, stearyl alcohol and cetearyl alcohol, classified by CTFA as "emulsion
stabilizers" agents.
[0028] Perfumes and fragrances may be included in the antiperspirant composition. Perfumes
give rise to an olfactory response in the form of a fragrance, and in addition may
contribute to mask body malodor.
[0029] Preservatives are required to prevent product damage caused by bacteria, yeast or
mold, and to protect the product from inadvertent contamination by the consumer during
use. Useful preservatives include sodium benzoate, ethylhexylglycerin and caprylyl
glycol, benzyl alcohol, methyl paraben, propyl paraben, DMDM hydantoin, methylchloroisothiaoline,
methylisothiazolinone, imidazolidinyl urea phenoxyethanol, sodium benzoate and benzoic
acid. EDTA and salts thereof are often used to further enhance preservation.
[0030] Antioxidants should be added to prevent formula from oxidation process. Useful antioxidants
include ascorbic acid, tocopheryl acetate and polypnehols. In the present invention,
anti-oxidants such as tocopheryl acetate (stabilized vitamin E) may be used as anti-oxidant
agent.
[0031] Humectants and moisturizing agents may be included in the composition. Suitable ingredients
include hydrophobic agents, hydrophilic agents and combinations thereof. Examples
of moisturizing agents are allantoin, glycerol, polyglycerylmethacrylate, panthenol,
polyols, ceramide, borage oil (linoleic acid), hyaluronic acid, sodium peroxylinecarbolic
acid (sodium PCA), wheat protein (e.g., laurdimonium hydroxypropyl hydrolyzed wheat
protein), hair keratin amino acids, panthenol; primrose oil; GLA 3 and other fish
oils that may include, for example, the omega-3 and omega-6 oils and/or linoleic acid;
and flax seed oil, and mixtures thereof. Other moisturizing agents can also be used.
[0032] Additionally, skin conditioners may be added to prevent or calm skin irritation.
For example, vegetable extracts may be added. Cotton milk (commercially available
from Symrise) may provide nourishing, calming and softening properties to skin. In
one embodiment, the composition of the invention contains about 34 to about 40 weight
percent milk proteins.
[0033] Pigments and colorants may be included in the antiperspirant composition of the present
invention.
[0034] Emollients, such as isopropylmyristate, mineral oils and vegetable oils in general,
which give rise to a tactile response in the form of an increase in skin lubricity
may be included for a more esthetically pleasing product. The composition may contain
emollients in any desired amount to achieve a desired emollient effect.
[0035] Non-volatile emollients are preferable in the present invention. Classes of non-volatile
emollients include non-silicone and silicone emollients. Non-volatile, non-silicone
emollients include C
12-15 alkyl benzoate. The non-volatile silicone material can be a polyethersiloxane, polyalkyarylsiloxane
or polyethersiloxane copolymer. An illustrative non-volatile silicone material in
the present invention is phenyl trimethicone. Non-limiting examples of emollients
can be found in
U.S. Pat. No. 6,007,799. Examples include, but are not limited to, PPG-14 butyl ether, PPG-15 stearyl ether,
PPG-3 myristyl ether, stearyl alcohol, stearic acid, glyceryl monoricinoleate, isobutyl
palmitate, glyceryl monostearate, isocetyl stearate, sulphated tallow, oleyl alcohol,
propylene glycol, isopropyl laurate, mink oil, sorbitan stearate, cetyl alcohol, hydrogenated
castor oil, stearyl stearate, hydrogenated soy glycerides, isopropyl isostearate,
hexyl laurate, dimethyl brassylate, decyl oleate, diisopropyl adipate, n-dibutyl sebacate,
diisopropyl sebacate, 2-ethyl hexyl palmitate, isononyl isononanoate, isodecyl isononanoate,
isotridecyl isononanoate, 2-ethyl hexyl palmitate, 2-ethyl hexyl stearate, Di-(2-ethyl
hexyl) adipate), Di-(2-ethyl hexyl) succinate, isopropyl myristate, isopropyl palmitate,
isopropyl stearate, octacosanol, butyl stearate, glyceryl monostearate, polyethylene
glycols, oleic acid, triethylene glycol, lanolin, castor oil, acetylated lanolin alcohols,
acetylated lanolin, petrolatum, isopropyl ester of lanolin, fatty acids, mineral oils,
butyl myristate, isostearic acid, palmitic acid, PEG-23 oleyl ether, olelyl oleate,
isopropyl linoleate, cetyl lactate, lauryl lactate, myristyl lactate, quaternised
hydroxy alkyl, aminogluconate, vegetable oils, isodecyl oleate, isostearyl neopentanoate,
myristyl myristate, oleyl ethoxy myristate, diglycol stearate, ethylene glycol monostearate,
myristyl stearate, isopropyl lanolate, paraffin waxes, glycyrrhizic acid, hydrocyethyl
stearate amide.
[0036] In one embodiment, the emollient is selected from linear silicones, cyclic silicones,
hydrocarbons, polyhydroxy alcohols having more than 3 carbon atoms, liquid or solid
polyalkyleneglycol ethers containing a polypropylene glycol (PPG) moiety and terminating
in an alkyl ether, and combinations thereof. In another embodiment, the emollient
is a volatile silicone having a flash point of 100° C. or less, such as cyclomethicone
or trisiloxane. In another embodiment, the emollient is a nonvolatile silicone, such
as dimethiconol or a longer chain dimethicone.
[0037] Surfactants and emulsifiers may be used in the antiperspirant compositions of the
invention. Typical surfactants are disclosed in
U.S. 2003/0007939A1. Emulsifiers useful in the composition include nonionic, anionic, cationic, amphoteric
or zwitterionic and blends thereof. Suitable emulsifiers are disclosed in
U.S. Patent No. 3,755,560 and
U.S. Patent No. 4,421,769. Examples are polyethylene glycol 20, sorbitan monolaurate (Polysorbate 20), polyethylene
glycol 20 stearyl ether (Brij 78, Steareth 20), polyethylene glycol ether of lauryl
alcohol (Laureth 23), polysorbate 80 (Tween 80), and lecithin.
[0038] Cellulosic gums also can be used as additives in the compositions of this invention.
Preferred cellulosic gums include water-soluble hydroxyalkylcellulose polymers such
as hydroxymethylcellulose, hydroxyethylcellulose and hydroxypropylcellulose. Other
thickening agents that may be used include acacia, agar, alginate, carrageenan, gum
tragacanth, xanthan gum, collagen, carboxypolymethylene, glyceryl monostearate, polyvinylpyrrolidone
and polyacrylamide.
[0039] The composition may be in the form of a solid or gel stick, cream, lotion, spray,
squeeze product, or the like, as known in the art.
[0040] Accordingly, the anticholinergic agent and other active agents may be contained in
a vehicle, as known in the art. The major types of antiperspirant vehicles most frequently
fall into the following categories: (a) solutions; (b) emulsions, both oil-in-water
and water-in-oil; and including lotions and creams; (c) suspensions; (d) gels; and
(e) solids and semi-solids including stick products. Antiperspirant products in some
vehicles, including liquids, gels, suspensions and emulsions, can be provided for
application via roll-on applicator, as known in the art.
[0041] Examples of solvents, in addition to water, that are frequently used in personal
care compositions are polypropylene glycol, polyethylene glycol, ethanol, glycerol,
ethylene glycol, 1,2,4-butanetriol, 1,2,6-hexanetriol, ethanol, isopropanol, butanetriol,
sorbitol esters, butanediol, butylene glycol, hexylene glycol, methylpropanediol,
pyrrolidone, N-methylpyrrolidone, dimethyl sulfoxide, dimethyl sulfone and similar
solvents and mixtures thereof.
[0042] The composition of the invention may be a squeeze product, including hydro-alcoholic
squeeze products.
[0043] The antiperspirant composition can be in gel form. A "gel" in accordance with the
present invention is a colloid in which the disperse phase has combined with the continuous
phase to produce a viscous, jelly-like product. Gels in accordance with the present
invention can be aqueous or nonaqueous. The gels will typically comprise a vehicle
comprising a gelling agent such as described above. The vehicle of the gels will also
typically comprise a solvent. A silicone surfactant may also be included required
to achieve stability.
[0044] Emulsions, such as lotions and creams, of the oil-in-water type and water-in-oil
type are well-known in the cosmetic art and are useful in the subject invention. Triphase
emulstions such as water-in-oil-in-water type may also be used. Oils useful in both
types of emulsions, and also for solvents in solvent-based vehicles in general, include
hydrocarbon oils and waxes (e.g., petrolatum, mineral oil, micro-crystalline waxes,
polyalkenes, paraffins, cerasin, ozokerite, polyethylene, perhydrosqualene, polyalphaolefins,
hydrogenated polyisobutenes and combinations thereof). Preferred are fatty acid derivatives,
cholesterol, cholesterol derivatives, diglycerides and triglycerides (e.g., castor
oil, soy bean oil, derivatized soybean oils such as maleated soy bean oil, safflower
oil, cotton seed oil, corn oil, walnut oil, peanut oil, olive oil, cod liver oil,
almond oil, avocado oil, palm oil, sesame oil, vegetable oils and vegetable oil derivatives,
sunflower seed oil, coconut oil and derivatized coconut oil, cottonseed oil and derivatized
cottonseed oil, jojoba oil, cocoa butter and combinations thereof, as well as any
of the aforementioned oils that have been partially or fully hydrogenated), acetoglyceride
esters (e.g., acetylated monoglycerides), alkyl esters, alkenyl esters (e.g., oleyl
myristate, oleyl stearate, oleyl oleate, and combinations thereof), lanolin and its
derivatives (e.g., lanolin, lanolin oil, lanolin wax, lanolin alcohols, lanolin fatty
acids, isopropyl lanolate, acetylated lanolin, acetylated lanolin alcohols, lanolin
alcohol linoleate, lanolin alcohol ricinoleate, hydroxylated lanolin, hydrogenated
lanolin and combinations thereof), wax esters (e.g., beeswax and beeswax derivatives,
spermaceti, myristyl myristate, stearyl stearate and combinations thereof), sterols
and phospholipids, and combinations thereof. Examples of alkyl esters include isopropyl
esters of fatty acids and long chain esters of long chain fatty acids, e.g., SEFA
(sucrose esters of fatty acids), pentaerythritol esters, aromatic mono, di or triesters,
cetyl ricinoleate, isopropyl palmitate, isopropyl myristate, cetyl ricinoleate and
stearyl ricinoleate. Other examples include hexyl laurate, isohexyl laurate, isohexyl
palmitate, decyl oleate, isodecyl oleate, hexadecyl stearate, decyl stearate, isopropyl
isostearate, diisopropyl adipate, diisohexyl adipate, dihexyldecyl adipate, diisopropyl
sebacate, acyl isononanoate lauryl lactate, myristyl lactate, cetyl lactate, and combinations
thereof. Still other suitable oils include milk triglycerides (e.g., hydroxylated
milk glyceride) and polyol fatty acid polyesters. Also useful are vegetable waxes
such as carnauba and candelilla waxes; sterols such as cholesterol, cholesterol fatty
acid esters; and phospholipids such as lecithin and derivatives, sphingo lipids, ceramides,
glycosphingo lipids, and combinations thereof.
[0045] The water-based roll-on is usually an oil-in-water emulsion rather than a water-in-oil
system due to the poorer efficiency of the latter. The oil-in-water emulsion presents
the active ingredient in a readily accessible solution form in the external phase.
Since the active ingredient ends up in the dissolved state, the formulator can use
either a liquid or solid antiperspirant active.
[0046] The composition of the invention may also be a clear water-in-oil roll-on. These
compositions are relatively new on the market. They demonstrate superior aesthetics
and leave no residue or deposit on the skin after application. Clarity is achieved
simply by following the room temperature order of addition specified.
[0047] The composition may alternatively be an aerosol. Sprays or aerosols have the advantage
of eliminating direct contact with hands for application. The propellant gas may be,
for example, a hydrocarbon (propane, isobutene), a chlorofluorocarbon, carbon dioxide
or nitrous oxide.
[0048] The composition of the invention may be a suspension.
[0049] In one embodiment, the composition is a lotion or a cream.
[0050] In another embodiment, the composition is a solid or semi-solid or stick, and comprises
an effective amount of anticholinergic agent and a solidifying agent, wherein the
composition is in the form of a solid or semi-solid at ambient temperature (e.g.,
25° C. and below). Accordingly, the composition may comprise for example mixtures
of waxes and oils and solutions based on aqueous, propylene glycol and/or alcohol
mixtures solidified for example by sodium stearate. Preferably, the solidifying agent
is selected from the group consisting of a wax and sodium stearate.
[0051] Solid compositions of the invention may also be finely divided and used in the form
of powders.
[0052] Almost all antiperspirant solids employ stearyl alcohol as the gelling agent. Emollients
are often added to impart a softer feel and to add glideability. Most solids also
contain talc and/or silica. Silica is an effective suspending agent that helps to
keep the active ingredient homogeneously suspended throughout the stick. Miscellaneous
ingredients often include colours, titanium dioxide (opacifying agent) and allantoin
(soothing agent).
[0053] Sticks and solids are complex chemical systems requiring a balance of ingredients
designed to make the most of several performance factors including payout, slip or
lubricity, chemical stability, softening temperature, and efficacy.
[0054] The composition of the invention may also be a foam. Accordingly, the liquid vehicles
described above may contain dispersions of gas in the liquid phase. The gas globules
may be of any size, from colloidal to macroscopic, as in soap bubbles. Typical liquid
foams are those used in shaving creams, etc.
EXAMPLES
Example 1
[0055] The following is composition is a hydro-alcoholic squeeze spray formulation of the
present invention.
TABLE 1
INGREDIENT |
FUNCTION |
% w/w |
A: SD Alcohol 40 |
Solvent |
38.00 |
B: Propylene glycol |
Humectant |
3.50 |
C: Deionized water |
Solvent |
48.00 |
D: Absorbents |
Absorbents |
6.00 |
E: Fragrance |
Perfume |
0.50 |
F: Acetyl octapeptide-3 or dipeptide diaminobutyroyl benzylamide diacetate |
Antiperspirant |
4.00 |
[0056] Procedure
- 1. Mix A and C using overhead stirrer
- 2. Add B. Mix for 10 min
- 3. Add D, E and F. When homogeneous, pour into suitable containers
Example 2
[0057] The following product is a water-in-oil emulsion according to the invention in which
the refractive indices of the continuous and dispersed phases are identically matched.
A silicone surfactant is used to achieve a stabile emulsion.
TABLE 2
INGREDIENT |
FUNCTION |
% w/w |
A: Cyclomethicone (and) Dimethicone Copolyol |
Solvent |
9.70 |
B: Cyclomethicone |
Solvent |
3.40 |
C: Dimethicone, 50 cst |
Skin Conditioning |
3.88 |
D: Isostearyl Palmitate |
Skin Conditioning |
2.42 |
E: Dipropylene Glycol |
Solvent |
19.51 |
F: Deionized Water |
Solvent |
50.69 |
G: Absorbents |
Absorbents |
6.00 |
H: Fragrance |
Perfume |
0.40 |
I: Acetyl octapeptide-3 or dipeptide diaminobutyroyl benzylamide diacetate |
Antiperspirant Agent |
4.00 |
[0058] Procedure
- 1. Combine A, B, C, D and H and mix until uniform
- 2. In a separate vessel combine E, F and G and mix until uniform
- 3. Match the refractive indexes of phases 1 and 2
- 4. Slowly add the aqueous phase from Step 2 to the oil phase from Step 1 and homogenize
at slow speed. The viscosity will slowly increase.
- 5. Add I and mix until uniform.
- 6. Homogenize vigorously (5000 rpm) until a firm gel is obtained (typically from 1
to 5 min)
- 7. Fill into airtight containers
Example 3
[0059] The following composition is an emulsion roll-on formulation according to the invention,
which exhibits excellent physical stability and application properties.
TABLE 3
INGREDIENT |
FUNCTION |
% w/w |
A: Steareth-21 |
Surfactant |
2.00 |
B: Steareth-2 |
Surfactant |
2.00 |
C: Steareth-5 Stearate |
Skin Conditioning |
1.00 |
D: Clyclomethicone (and) PPG-15 Stearyl Ether |
Skin Conditioning |
5.00 |
E: Deionized Water |
Solvent |
79.20 |
F:Absorbents |
Absorbents |
6.00 |
G: Fragrance |
Perfume |
0.80 |
H: Acetyl octapeptide-3 or dipeptide diaminobutyroyl benzylamide diacetate |
Antiperspirant Agent |
4.00 |
[0060] Procedure
- 1. Combine A, B, C and D and heat to 700° C
- 2. Heat E separately at 700° C
- 3. Add A, B, C and D to E with agitation
- 4. Homogenize the mixture for 1-3 min
- 5. Cool to 35° C with continuous agitation
- 6. Add F to emulsion slowly with agitation
- 7. Add H and G with agitation
- 8. Homogenize the mixture again for 1-3 min
- 9. Fill into suitable containers
Example 4
[0061] This composition according to the invention provides superior aesthetics and leaves
no residue or deposit on the user's skin after application. It is a clear antiperspirant
product made with the following ingredients using the order of addition below at room
temperature (20 -22° C).
TABLE 4
INGREDIENT |
FUNCTION |
% w/w |
A: Deionized Water |
Solvent |
8.75 |
B: Dipropylene Glycol |
Solvent |
3.00 |
C: PEG-7 Glyceryl Cocoate |
Skin Conditioning |
18.20 |
D: Cyclomethicone (and) Dimethicone Copolyol |
Skin Conditioning |
41.50 |
E: Cetearyl Octanoate |
Surfactant |
3.20 |
F: Polysorbate 20 |
Surfactant |
1.00 |
G: Deionized Water |
Solvent |
12.60 |
H: Isopropyl Myristate |
Skin Conditioning |
1.00 |
I: Absorbents |
Absorbents |
6.00 |
J: Fragrance |
Perfume |
0.75 |
K: Acetyl octapeptide-3 or dipeptide diaminobutyroyl benzylamide diacetate |
Antiperspirant Agent |
4.00 |
[0062] Procedure
- 1. Combine A and B with overhead mixing (medium agitation)
- 2. Slowly add C. Mix well
- 3. Slowly add D. Mix well
- 4. Slowly add E and F. Mix well
- 5. Premix H and I. Slowly add to the main batch
- 6. Slowly add G. Mix well
- 7. Slowly add K and J. Mix well until clear
- 8. Pour into appropriate containers
Example 5
[0063] A composition of the invention in aerosol form is made by the following procedure:
TABLE 5
INGREDIENT |
FUNCTION |
% w/w |
A: Bentone Gel VS-5 PC |
Suspending Agent |
18.50 |
B: Cyclomethicone |
Solvent |
21.20 |
C: Dimethicone, 50 cst |
Skin Conditioning |
8.50 |
D: Isopropyl Myristate |
Skin Conditioning |
1.50 |
E: Absorbents |
Absorbents |
6.00 |
F: Fragrance |
Perfume |
0.30 |
G: Acetyl octapeptide-3 or dipeptide diaminobutyroyl benzylamide diacetate |
Antiperspirant Agent |
4.00 |
H: Isobutane |
Propellant |
40.00 |
[0064] Procedure
- 1. Combine A, B, C and D. Mix well for about 10 min or until homogeneous.
- 2. Add E mix until uniform
- 3. Add G mix until uniform
- 4. Add F and mix 5 min
- 5. Place mixture into a suitable container and charge with H as specified.
Example 6
[0065] The following composition according to the invention is a solid formulation.
TABLE 6
INGREDIENT |
FUNCTION |
% w/w |
A: Volatile Silicone |
Solvent |
56.70 |
B: Stearyl Alcohol |
Surfactant |
20.00 |
C: PPG-3 Myristyl Ether |
Skin Conditioning |
5.00 |
D: PEG-8 Distearate |
Surfactant |
2.00 |
E: Talc |
Absorbent |
1.00 |
F: Silica |
Absorbent |
1.50 |
G: Polyethylene |
Film Former |
3.00 |
H: Absorbents |
Absorbents |
6.00 |
I: Fragrance |
Perfume |
0.80 |
J: Acetyl octapeptide-3 or dipeptide diaminobutyroyl benzylamide diacetate |
Antiperspirant Agent |
4.00 |
[0066] Procedure
- 1. Heat A to 65° C
- 2. Add C and D with stirring
- 3. Add B slowly. Maintain 65° C
- 4. Add E, F, G and H.
- 5. Cool to 60°C. Add I and J.
- 6. Pour into stick casings at 54°C.
Example 7
[0067] Using the ingredients in Table 7 and the procedure below, a comparative roll-on composition
containing acetyl hexapeptide-8 was prepared.
TABLE 7
INGREDIENT |
FUNCTION |
% w/w |
A: Aqua |
Solvent |
79.51 |
B: Steareth-2 |
Surfactant |
3.00 |
C: Steareth-21 |
Surfactant |
1.00 |
D: PPG-15 Stearyl Ether |
Emollient |
4.00 |
E: Ethylhexyglycerin; Caprylyl Glycol |
Skin Conditioning Agent |
1.00 |
F: Polyglyceryl-3 Caprylate |
Emulsifying Agent |
0.30 |
G: Citric acid |
pH adjuster |
0.68 |
H: Sodium Hydroxide |
pH adjuster |
0.01 |
I: Sodium Benzoate |
Preservative |
0.50 |
J: Acetyl Hexapeptide-8 |
Antiperspirant agent |
10.00 |
[0068] Procedure:
- 1. Oily Phase: Combined B, C, D, E and F in an auxiliary tank. Started heating to
75-80°C.
- 2. Water Phase: Combined A and I in a main tank. Started heating to 75°-80°C.
- 3. Emulsification Step: Added oily phase over water phase (both 75-80°C). Mixed for
5 min. Homogenized for 4 min.
- 4. Cooling Step: Cooled the emulsion to 25° C. Added G, H and J. Mixed for 10 min.
Example 8
[0069] Using the ingredients in Table 8 and the procedure below, a roll-on composition containing
acetyl cctapeptide-3 according to the invention was prepared.
TABLE 8
INGREDIENT |
FUNCTION |
% w/w |
A: Aqua |
Solvent |
79.51 |
B: Steareth-2 |
Surfactant |
3.00 |
C: Steareth-21 |
Surfactant |
1.00 |
D: PPG-15 Stearyl Ether |
Emollient |
4.00 |
E: Ethylhexyglycerin; Caprylyl Glycol |
Skin Conditioning Agent |
1.00 |
F: Polyglyceryl-3 Caprylate |
Emulsifying Agent |
0.30 |
G: Citric acid |
pH adjuster |
0.68 |
H: Sodium Hydroxide |
pH adjuster |
0.01 |
I: Sodium Benzoate |
Preservative |
0.50 |
J: Acetyl Octapeptide-3 |
Antiperspirant agent |
10.00 |
[0070] Procedure:
- 1. Oily Phase: Combined B, C, D, E and F in an auxiliary tank. Started heating to
75-80° C.
- 2. Water Phase: Combined A and I in a main tank. Started heating to 75°-80° C.
- 3. Emulsification Step: Added oily phase over water phase (both 75-80 °C). Mixed for
5 min. Homogenized for 4 min.
- 4. Cooling Step: Cooled the emulsion to 25° C. Add G, H and J. Mixed it for 10 min.
Example 9
[0071] Using the ingredients in Table 9 and the procedure below, a roll-on composition containing
dipeptide diaminobutyroyl benzylamide diacetate according to the invention was prepared.
TABLE 9
INGREDIENT |
FUNCTION |
% w/w |
A: Aqua |
Solvent |
84.46 |
B: Steareth-2 |
Surfactant |
3.00 |
C: Steareth-21 |
Surfactant |
1.00 |
D: PPG-15 Stearyl Ether |
Emollient |
4.00 |
E: Ethylhexyglycerin; Caprylyl Glycol |
Skin Conditioning Agent |
1.00 |
F: Polyglyceryl-3 Caprylate |
Emulsifying Agent |
0.30 |
G: Citric acid |
pH adjuster |
0.73 |
H: Sodium Hydroxide |
pH adjuster |
0.01 |
I: Sodium Benzoate |
Preservative |
0.50 |
J: Dipeptide Diaminobutyroyl Benzylamide Diacetate |
Antiperspirant agent |
5.00 |
[0072] Procedure:
- 1. Oily Phase: Combined B, C, D, E and F in an auxiliary tank. Started heating to
75-80° C.
- 2. Water Phase: Combined A and I in a main tank. Started heating to 75-80° C.
- 3. Emulsification Step: Added oily phase over water phase (both 75-80° C). Mixed for
5 min. Homogenized for 4 min.
- 4. Cooling Step: Cooled the emulsion to 25° C. Added G, H and J. Mixed it for 10 min.
Example 10
[0073] An
in vivo study of the eight-hour antiperspirant efficacy of the compositions of Examples 7,
8 and 9 was performed as follows using the US FOOD AND DRUG ADMINISTRATION Guidelines
for Effectiveness Testing of OTC Antiperspirant Drug Products, 2003. Example 7 was
comparative, as indicated above.
[0074] Fifteen subjects were used to test each composition. Subjects were first subjected
to a 21-day conditioning period, which began with a 14 day wash out period. During
14 day wash out period, the subjects used a standard bar soap and bacteriostatic deodorant
supplied by the institute running the study. The subjects did not remove underarm
hair. Following this, from day 15 to day 21 the subjects were instructed to use only
standard soap and discontinue the bacteriostatic deodorant.
[0075] During the conditioning period, subjects were instructed and supervised by a trained
technician to wash their underarms according to the following procedure: a) wash one
of the underarms for 10 seconds with an aqueous solution of standard soap 2.0%; b)
rinse thoroughly with running water until the soap is completely removed; c) dry the
underarm with a paper towel; and d) repeat the procedure with the other underarm.
[0076] After the wash out period was completed, each subject was checked for unauthorized
use of antiperspirant products during the conditioning period using a cotton swab
in the underarms.
[0077] Next, a 30 day application period began. 150 cm
2, randomly distributed areas were marked on each subjects' underarm. Test samples
were then applied to one underarm of each subject, while the other underarm was untreated
as a control every day during the 30 day application period. Subjects waxed or shaved
their underarms every Friday evening.
[0078] On day 30 of the 30 day application period, each subject was provided with a 100%
cotton t-shirt previously washed with water and neutral soap without fragrance and
again washed only with water. The subjects were instructed to wear the T-shirts for
eight hours.
[0079] After eight hours, the subjects were placed in a room at 37.8° C ± 1° C and relative
humidity between 30% and 40% for 80 minutes. After 40 minutes in the hot room, pads
previously weighed and stored in closed polyethylene bags were removed from the bags
and placed immediately onto the subjects' underarms, and then replaced every 20 minutes.
Subjects ingested 200 mL of water when entering the hot room and also 40 minutes later
in order to maintain the internal level of hydration, allowing the sweat to flow freely
and evidencing only the effects of the formulation of the product tested. The initial
40 minute period was considered as an acclimatization period.
[0080] Used pads were collected every 20 minutes and weighed. The weights of the pads pre-
and post-use were compared according to the FDA Guidelines using statistical analysis
with the Wilcoxon Signed Rank test (FDA protocol) and the Student-t test paired with
the unilateral hypothesis of improvement for sweating assessment. The confidence level
considered in the comparative analysis was 95%. Software: XLSTAT 2013 and MINITAB
14.
[0081] The results are shown in Table 10.
TABLE 10
Anticholinergic Agent |
% of subjects with reduction in relation to control |
Average % of sweat reduction (mg) |
Acetyl Hexapeptide-8 |
66.7 |
8.0% |
Acetyl Octapeptide-3 |
81.8 |
20.7 |
Diaminobutyroyl Benzylamide Diacetate |
92.3 |
25.6 |
[0082] The compositions containing acetyl octapeptide-3 and dipeptide diaminobutyroyl benzylamide
diacetate according to the invention reduced the sweat by an average of 20.7% and
25.6%, respectively, relative to the control for at least 50% of subjects (81.8% and
92.3%). This confirms antiperspirant activity. The FDA Guidelines call for a minimum
of 20% sweat reduction in at least 50% volunteers. In contrast, the comparative composition
containing acetyl hexapeptide-8 showed sweat reduction by an average of only 8.0%
relative to the control, which did not meet success criteria.